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Separating and purifying method of acarbose

An acarbose, separation and purification technology, applied in chemical instruments and methods, sugar derivatives, sugar derivatives, etc., can solve the problem of low yield, and achieve simple and convenient separation methods, high yields, and high yields. stable effect

Inactive Publication Date: 2018-06-12
SUZHOU NANOMICRO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Patent CN200310117484 discloses the purification method of acarbose, using three-step membrane separation and one-step chromatography resin, and the yield of high-purity (>99%) products is not high

Method used

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  • Separating and purifying method of acarbose
  • Separating and purifying method of acarbose
  • Separating and purifying method of acarbose

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] 567ml crude acarbose (45.25% purity), filtered with a filter membrane with a pore size of 8μm, collected the filtrate, and adjusted its pH to 5.05 with 0.5N hydrochloric acid. A 16×405mm chromatographic column, UniAcarbose GIII microspheres (manufactured by Suzhou Nanomicro Technology Co., Ltd.) was used as the chromatographic column packing, and the packed column volume was 81ml. Before loading the sample, equilibrate the column with ultrapure water, and then load the acarbose solution after the above treatment into the column containing UniAcarboseGIII microspheres at a flow rate of 3-7 times the column volume per hour. Chromatography was performed, and then 0.5N hydrochloric acid solution was used for elution. The solution of the target peak is collected in sections, and the components that meet the requirements are summarized. After high performance liquid chromatography analysis, the purity of acarbose in the eluent is above 99.7%, and the yield is 86%.

[0042] figu...

Embodiment 2

[0050] 156ml crude acarbose (40.958% purity), filtered with a filter membrane with a pore size of 8μm, collected the filtrate, and adjusted its pH to 5.01 with 0.5N hydrochloric acid. A 16x260mm chromatographic column, UniAcarbose GIII microspheres (manufactured by Suzhou Nanomicro Technology Co., Ltd.) as the chromatographic column packing, with a packing volume of 52ml. Before loading the sample, equilibrate the chromatography column with deionized water, and then load the sample at a flow rate of 3-7 times the column volume per hour, and then use 0.5N hydrochloric acid solution for elution. The solution of the target peak is collected in sections, and the components that meet the requirements are summarized. After high performance liquid chromatography analysis, the purity of acarbose in the eluent is over 99.3%, and the yield is 85%.

Embodiment 3

[0052] 567ml crude acarbose (43.504% purity), filtered with a filter membrane with a pore size of 8μm, collected the filtrate, and adjusted its pH to 5.08 with 0.5N hydrochloric acid. A 16×405mm chromatographic column, UniAcarbose GIII microspheres (manufactured by Suzhou Nanomicro Technology Co., Ltd.) was used as the chromatographic column packing, and the packed column volume was 81ml. Before loading the sample, equilibrate the chromatography column with deionized water, and then load the sample at a flow rate of 3-7 times the column volume per hour, and then use 0.5N hydrochloric acid solution for elution. The solution of the target peak is collected in sections, and the components that meet the requirements are summarized. After high performance liquid chromatography analysis, the purity of acarbose in the eluent is over 99.1%, and the yield is 82%.

[0053] The present invention uses monodisperse polystyrene / divinylbenzene ion chromatography medium as the exchange filler, a...

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Abstract

The invention provides a high-efficient separating and purifying method of acarbose. The method comprises the following steps of filtering an acarbose solution, adjusting a pH value of the solution, loading a treated acarbose solution sample into an ion-exchange chromatography medium full of monodisperse polystyrene / divinyl benzene, carrying out chromatography, adopting a hydrochloric acid solution as a flow phase for eluting a target product, and collecting a target solution to obtain a high-purity acarbose solution. According to the purifying method, only one-step purification is needed, only hydrochloric acid water solution is utilized during an eluting and regenerating process, no other organic solvent is involved, after purifying, the purity can reach to 99 percent or more, the totalyield is 80 percent or more, and the method is suitable for industrial production.

Description

Technical field [0001] The invention relates to the field of medicine purification, in particular to a method for separating and purifying acarbose. Background technique [0002] Acarbose is the first alpha-glucosidase inhibitor for clinical use developed by Bayer in Germany in the mid-1970s. Its mechanism of action is the same as that of Miglito and Voggle. Voglibose. It was first marketed in Germany in 1990, and was approved by the FDA in 1996 to be marketed in the United States. Acarbose is a new drug for the treatment of type II diabetes, and it is also used to treat metabolic disorders such as hyperglycemia and obesity. [0003] The sugar chemical structure of acarbose is relatively complex, and the current industrial scale is obtained through microbial fermentation. In 1977, Bayer obtained acarbose from the metabolites of Actinoplanes sp (Actinoplanes sp) SE50, SE82, and SE18. In 1994, "Baitang Ping" was used to treat mild and moderate type II diabetes, and other anti-diabe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/203C07H1/06
CPCC07H1/06C07H15/203
Inventor 江必旺石凌超邹胜张彦辉
Owner SUZHOU NANOMICRO TECH CO LTD
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